General Information of Drug Combination (ID: DCKPLK7)

Drug Combination Name
MK-1775 Erlotinib
Indication
Disease Entry Status REF
Germ cell tumour Investigative [1]
Component Drugs MK-1775   DM3WDZ5 Erlotinib   DMCMBHA
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: PA1
Zero Interaction Potency (ZIP) Score: 4.89
Bliss Independence Score: 5.86
Loewe Additivity Score: 1.6
LHighest Single Agent (HSA) Score: 7.33

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of MK-1775
Disease Entry ICD 11 Status REF
Ovarian cancer 2C73 Phase 2 [2]
Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
MK-1775 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Wee1-like protein kinase (WEE1) TTJFOAL WEE1_HUMAN Inhibitor [7]
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MK-1775 Interacts with 2 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Decreases Phosphorylation [6]
Cellular tumor antigen p53 (TP53) OTIE1VH3 P53_HUMAN Increases Response To Substance [6]
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Indication(s) of Erlotinib
Disease Entry ICD 11 Status REF
Adrenal gland neoplasm N.A. Approved [4]
Adult hepatocellular carcinoma N.A. Approved [4]
Brain cancer 2A00 Approved [4]
Esophageal disorder N.A. Approved [4]
Lung cancer 2C25.0 Approved [4]
Non-small-cell lung cancer 2C25.Y Approved [5]
Pancreatic adenocarcinoma N.A. Approved [4]
Psoriasis EA90 Approved [4]
Salivary gland squamous cell carcinoma N.A. Approved [4]
Pancreatic cancer 2C10 Phase 3 [5]
Colon cancer 2B90.Z Phase 2 [5]
Ependymoma 2A00.0Y Investigative [4]
Neoplastic meningitis N.A. Investigative [4]
Neuroblastoma 2D11.2 Investigative [4]
Erlotinib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Inhibitor [8]
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Erlotinib Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [10]
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Erlotinib Interacts with 4 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [11]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Metabolism [12]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [12]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [12]
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Erlotinib Interacts with 1 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Increases Response [13]
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Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Adenocarcinoma DC92V49 CAOV3 Investigative [1]
Adenocarcinoma DCTO1SJ NCIH1650 Investigative [1]
Adenocarcinoma DCEZJXP NCIH2122 Investigative [1]
Adenocarcinoma DCK3IEP NCIH520 Investigative [1]
Adenocarcinoma DCDA56W COLO320DM Investigative [1]
Adenocarcinoma DCMFK7Q HCT116 Investigative [1]
Adenocarcinoma DCJ3FI1 HT29 Investigative [1]
Adenocarcinoma DCHY8DA SW-620 Investigative [1]
Amelanotic melanoma DC7CN19 A2058 Investigative [1]
Ewing sarcoma-peripheral primitive neuroectodermal tumour DCVEAFS ES2 Investigative [1]
Large cell lung carcinoma DC8JI6U NCI-H460 Investigative [1]
Malignant melanoma DCOEWRR A375 Investigative [1]
Malignant melanoma DC45ENQ SKMEL30 Investigative [1]
Malignant melanoma DCMV16H UACC62 Investigative [1]
Mesothelioma DC9QV02 MSTO Investigative [1]
Ovarian endometrioid adenocarcinoma DCEG4FJ A2780 Investigative [1]
Prostate carcinoma DCWS8F2 VCAP Investigative [1]
Breast and ovarian cancer syndrome DCVTOT1 UWB1289+BRCA1 Investigative [14]
Breast carcinoma DCBHNVH KPL1 Investigative [14]
Breast carcinoma DCKLEMV OCUBM Investigative [14]
Carcinoma DCZLMSY EFM192B Investigative [14]
Colon adenocarcinoma DCANMCQ LOVO Investigative [14]
Colon carcinoma DCVL1HK RKO Investigative [14]
Rectal adenocarcinoma DCFIU4D SW837 Investigative [14]
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⏷ Show the Full List of 24 DrugCom(s)

References

1 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7702).
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Erlotinib FDA Label
5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4920).
6 Functional kinomics identifies candidate therapeutic targets in head and neck cancer. Clin Cancer Res. 2014 Aug 15;20(16):4274-88. doi: 10.1158/1078-0432.CCR-13-2858.
7 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
8 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
9 Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice. Mol Cancer Ther. 2008 Aug;7(8):2280-7.
10 Functions of the breast cancer resistance protein (BCRP/ABCG2) in chemotherapy. Adv Drug Deliv Rev. 2009 Jan 31;61(1):26-33.
11 In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9.
12 Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706.
13 Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med. 2004 May 20;350(21):2129-39. doi: 10.1056/NEJMoa040938. Epub 2004 Apr 29.
14 Biologically active neutrophil chemokine pattern in tonsillitis.Clin Exp Immunol. 2004 Mar;135(3):511-8. doi: 10.1111/j.1365-2249.2003.02390.x.